Synthesis and structure-activity relationships of a series of novel thiazoles as inhibitors of aminoacyl-tRNA synthetases

X Y Yu; J M Hill; G Yu; W Wang; A F Kluge; P Wendler; P Gallant

doi:10.1016/s0960-894x(98)00738-0

Synthesis and structure-activity relationships of a series of novel thiazoles as inhibitors of aminoacyl-tRNA synthetases

Bioorg Med Chem Lett. 1999 Feb 8;9(3):375-80. doi: 10.1016/s0960-894x(98)00738-0.

Authors

X Y Yu¹, J M Hill, G Yu, W Wang, A F Kluge, P Wendler, P Gallant

Affiliation

¹ Department of Medicinal Chemistry, Cubist Pharmaceuticals, Inc., Cambridge, MA 02139, USA.

PMID: 10091687
DOI: 10.1016/s0960-894x(98)00738-0

Abstract

A series of novel aminoacyl adenylate mimics has been prepared and evaluated for their inhibitory activity against aminoacyl-tRNA synthetases. Several of these thiazole derivatives displayed potent and selective enzyme activity against both Gram-positive and Gram-negative bacteria.

MeSH terms

Amino Acyl-tRNA Synthetases / antagonists & inhibitors*
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Escherichia coli / enzymology
Humans
Staphylococcus aureus / enzymology
Structure-Activity Relationship
Thiazoles / chemical synthesis*
Thiazoles / chemistry
Thiazoles / pharmacology*

Substances

Enzyme Inhibitors
Thiazoles
Amino Acyl-tRNA Synthetases